BIOPHARMACEUTICS

Introduction to bipharmaceutics:
Biopharmaceutics: the study of how the
physicochemical properties of drugs, dosage
forms and routes of administeration affect the
rate and extent of the drug absorption.
Thus, biopharmaceutics involves factors that
influence the:
1) protection and stability of the drug within the
product;
2) the rate of drug release from the product;
3) the rate of dissolution of the drug at the
absorption site; and
4) the availability of the drug at its site of action .
Introduction to bipharmaceutics (Cont.):
Scheme demonstrating the dynamic relationships
among the drug, the product, and pharmacologic
effect.
Introduction to bipharmaceutics (Cont.):
ADME: is an acronym in pharmacokinetics and
pharmacology for absorption, distribution, metabolism,
and excretion, and describes the disposition of a
pharmaceutical compound within an organism.

Pharmacokinetics: The study and characterization of

the time course (kinetics) of drug absorption, distribution,
metabolism and elimination (ADME).
Introduction to bipharmaceutics (Cont.):

Absorption: is the process of a substance entering the

body.
Distribution: is the dispersion of substances throughout
the fluids and tissues of the body.
Metabolism: is the irreversible transformation of parent
compounds into daughter metabolites.
Excretion: is the elimination of the substances from the
body.
Introduction to bipharmaceutics (Cont.):
Introduction to bipharmaceutics (Cont.):
Introduction to bipharmaceutics (Cont.):
Bioavailability: The rate and extent of drug absorption.
Bioavailable dose: The fraction of an administered
dose of a particular drug that reaches the systemic
circulation intact.
Plasma level-time curve:
Introduction to bipharmaceutics (Cont.):
The plasma level-time curve is generated
by measuring the drug concentration in
plasma samples taken at various time
intervals after a drug product is
administered.

The concentration of drug in each plasma

sample is plotted against the corresponding
time at which the plasma sample was
removed.
Introduction to bipharmaceutics (Cont.):
Introduction to bipharmaceutics (Cont.):
Drug Product Performance Parameters:
1- Minimum effective concentration (MEC): The minimum
concentration of drug needed at the receptors to produce
the desired pharmacologic effect.

2- Minimum toxic concentration (MTC): The drug

concentration needed to just produce a toxic effect.

3- Onset time: The time required for the drug to reach the
MEC.

4- Duration of action: The difference between the onset

time and the time for the drug to decline back to the MEC.
Introduction to bipharmaceutics (Cont.):
5- The time of peak plasma level: The time of
maximum drug concentration in the plasma and
is proportional to the rate of drug absorption.

6- The peak plasma level: The maximum drug

concentration, usually related to the dose and the
rate constants for absorption and elimination of
the drug.

7- Area under the curve: It is related to the

amount of drug absorbed systemically.
Bioavailability and Bioequivalence:
It is the fraction of the drug absorbed through non-
intravenous administration compared with the
corresponding intravenous administration of the same
drug.
Bioavailability and Bioequivalence:
Relative bioavailability:
This measures the bioavailability (estimated as area under
the curve, or AUC) of a certain drug when compared with
another formulation of the same drug, usually an
established standard, or through administration via a
different route.
Bioavailability and Bioequivalence:
Bioequivalence:
- means pharmaceutical equivalents or pharmaceutical
alternatives whose rate and extent of absorption do not
show a significant difference when administered at the
same molar dose of the therapeutic moiety under similar
experimental conditions.

- Bioequivalence studies are usually performed to compare

the rate and/or extent of absorption of a new drug product
or a generic equivalent with that of a recognized standard.

-
Bioavailability and Bioequivalence:
Two dosage forms are Two dosage forms are
bioequivalent: not bioequivalent:
 Bioavailability and Bioequivalence:
- Pharmaceutical Alternatives:
means drug products that contain the identical therapeutic moiety, or
its precursor, but not necessarily in the same amount or dosage form
or as the same salt or ester.
- Pharmaceutical Equivalent:
means drug products that contain identical amounts of the identical
active drug ingredient, i.e., the salt or ester of the same therapeutic
moiety, in identical dosage forms, but not necessarily containing the
same inactive ingredients, and that meet the identical compendial or
other applicable standard of identity, strength, quality, and purity,
including potency and where applicable, content uniformity,
disintegration times and/or dissolution rate.

- Brand Name: is the trade name of the drug.

- Chemical Name: is the name used by the organic chemist to indicate

the chemical structure of the drug.

- Generic Name: is the established, non proprietary or common name of

the active drug in a drug product.
Bioavailability and Bioequivalence:
Methods to Assess Bioavailability:
I. Dissolution at administration or absorption site:
Method of evaluation: Dissolution rate
Example: In vitro: water, buffer, artificial gastric fluid, artificial
intestinal fluid, artificial saliva, artificial rectal fluid.
II.Free drug in systemic circulation:
Method of evaluation: 1.Blood level time profile
2.Peak blood level
3.Time to reach peak
4.Area under blood level time curve
Example: In vivo: whole blood, plasma, serum
Bioavailability and Bioequivalence:
III. Pharmacologic effect:
Method of evaluation: 1.Onset of effect
2.Duration of effect
3.Intensity of effect
Example: In vivo: discriminate measurement of
pharmacologic effect (blood pressure, blood sugar, blood
coagulation time)
IV. Clinical response:
Method of evaluation: 1.Controlled clinical blind or double-
blind study
2.Observed clinical success or failure
Example: In vivo: evaluation of clinical responses
Bioavailability and Bioequivalence:
V. Elimination:
Method of evaluation: 1.Cumulative amount of drug excreted
2.Maximum excretion rate
3.Peak time of excretion
Example: In vivo: urine